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Inhibition of tubulin polymerization in human HCT-116 cells

PubChem AID
1952418
Primary Citation
Exploration of cytotoxic potential and tubulin polymerization inhibition activity of cis-stilbene-1,2,3-triazole congeners [PMID: 36970147]
Source
External ID
BioAssay Type
Confirmatory
Tested Substances
Tested Compounds
Version
1.1
Status
Live
Dates
  • Deposit:
    2024-05-03
  • Modify:
    2024-05-03
Description
This bioassay record (AID 1952418) reports results from the above primary citation. Additional data from the same publication are reported in a total of 46 BioAssay records in PubChem.

1 Description

Title: Exploration of cytotoxic potential and tubulin polymerization inhibition activity of cis-stilbene-1,2,3-triazole congeners.

Abstract: To scrutinize cis-stilbene based molecules with potential anticancer and tubulin polymerization inhibition activity, a new series of cis-stilbene-1,2,3-triazole congeners was designed and synthesized via a click chemistry protocol. The cytotoxicity of these compounds 9a-j and 10a-j was screened against lung, breast, skin and colorectal cancer cell lines. Based on the results of MTT assay, we further evaluated the selectivity index of the most active compound 9j (IC50 3.25 ± 1.04 μM on HCT-116) by comparing its IC50 value (72.24 ± 1.20 μM) to that of the normal human cell line. Further, to confirm apoptotic cell death, cell morphology and staining studies (AO/EB, DAPI and Annexin V/PI) were carried out. The outcomes of studies showed apoptotic features like change in cell shape, cornering of nuclei, micronuclei formation, fragmented, bright, horseshoe-shaped nuclei, etc. Moreover, active compound 9j displayed G2/M phase cell cycle arrest with significant tubulin polymerization inhibition activity with an IC50 value of 4.51 μM. Additionally, in silico ADMET, molecular docking and molecular dynamic studies of 9j with 3E22 protein proved the binding of the compound at the colchicine binding site of tubulin.

2 Comment

Compounds with activity <= 10uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Journal: RSC Med Chem

Year: 2023

Volume: 14

Issue: 3

First Page: 482

Last Page: 490

DOI: 10.1039/d2md00400c

Target ChEMBL ID: CHEMBL2095182

ChEMBL Target Name: Tubulin

ChEMBL Target Type: PROTEIN COMPLEX GROUP - Target is a poorly defined protein complex, where subunit composition is unclear (e.g., GABA-A receptor)

Relationship Type: D - Direct protein target assigned

Confidence: Multiple direct protein targets may be assigned

3 Result Definitions

4 Data Table

5 Target

3 of 15
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9 of 15
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8 Identity

8.1 BioAssay Name

Inhibition of tubulin polymerization in human HCT-116 cells

8.2 Source

8.3 External ID

8.4 Project Category

Literature, Extracted

8.5 BioAssay Type

Confirmatory

8.6 Deposit Date

2024-05-03

8.7 Modify Date

Version 1.1
2024-05-03 (currently shown)

8.8 Status

Live

9 Same-Publication BioAssays

10 BioAssay Annotations

Assay Format
Cell-based
Assay Type
Binding
Assay Cell Type
HCT-116
Assay Organism

11 Information Sources

  1. PubChem
  2. ChEMBL
    LICENSE
    Access to the web interface of ChEMBL is made under the EBI's Terms of Use (http://www.ebi.ac.uk/Information/termsofuse.html). The ChEMBL data is made available on a Creative Commons Attribution-Share Alike 3.0 Unported License (http://creativecommons.org/licenses/by-sa/3.0/).
    http://www.ebi.ac.uk/Information/termsofuse.html
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